Practical and Asymmetric Synthesis of Apremilast Using Ellman’s Sulfinamide as a Chiral Auxiliary

Molbank

卷:2021

Bofei Wang¹  Fangrui Zhong¹ 

[1] School of Chemistry and Chemical Engineering, Huazhong University of Science and Technology (HUST), Luoyu Road 1037, Wuhan 430074, China;

关键词: apremilast;    asymmetric synthesis;    Ellman’s sulfinamide;    chiral auxiliary;   

DOI  :  10.3390/M1275

来源: DOAJ

【 摘 要 】

Herein, we described a new protocol for the asymmetric synthesis of apremilast using tert-butanesulfinamide as a chiral auxiliary. This synthetic route consisted of four steps starting from the commercially available 3-hydroxy-4-methoxybenzaldehyde, and apremilast was accordingly obtained in an overall 56% yield and with 95.5% ee.

【 授权许可】

Unknown